Topical Vitamin C and Its Derivatives in Cosmetic Science: Stability, Efficacy, and Formulation Strategies

Abstract

Context: Vitamin C and its derivatives are extensively incorporated into cosmetic formulations owing to their antioxidant properties, stimulation of collagen synthesis, and capacity to improve hyperpigmentation. Although numerous experimental and formulation-oriented studies have assessed the performance of various vitamin C derivatives, current evidence reveals considerable variability in their stability, penetration, and enzymatic conversion. However, comprehensive overviews that systematically summarize and compare these characteristics remain scarce. Although these derivatives share similar biological functions, their topical efficacy varies significantly because differences in molecular structure affect stability, solubility, dermal absorption, and overall biological activity. Evidence Acquisition: This review presents a concise comparison of commonly used topical vitamin C derivatives to facilitate more informed formulation decisions in cosmetic products. The extracted information includes physicochemical stability, enzymatic conversion to L-ascorbic acid (L-AA), antioxidant capacity, collagen-stimulating potential, and anti-melanogenic effects. Results: The findings indicate that L-AA demonstrates the most potent direct biological activity but is constrained by poor stability and limited skin penetration. Water-soluble derivatives, such as magnesium ascorbyl phosphate (MAP) and sodium ascorbyl phosphate (SAP), offer enhanced stability and lower irritation potential but require enzymatic activation. Lipophilic derivatives, including ascorbyl tetraisopalmitate, provide superior skin permeability and sustained antioxidant or brightening activity, whereas glucoside-based and amphiphilic derivatives exhibit moderate penetration with notable photoprotective and anti-inflammatory effects. Conclusions: Overall, no single derivative is universally superior; optimal selection depends on aligning each derivative’s physicochemical profile with the intended formulation objectives and desired cosmetic outcomes.